ATX968 | ATX968 : Inhibitor of DHX9
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
In Vivo
Control Compounds
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DHX9
  • Kd:1.3 ± 0.3 nM
  • IC50:8 ± 3 nM
  • EC50:101 nM
  • EC50:95 nM
  • EC50:236 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
A screen of 97 kinases (KINOMEscanEDGE™) was performed by Eurofins DiscoverX Corporation. ATX968 was ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
ATX968 was profiled in a large panel of cancer cell lines from multiple lineages in a 10-day prolife ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
ATX968 does not significantly inhibit DHX36, SMARCA2 or WRN helicase activity (measured by ADP-Glo™ ...

Potency
Cellular
In Vitro

DHX9

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-24-0397

Chemical Information

Molecular Formula C18H16ClN3O3S2
SMILEs Cc1cccnc1-c1csc(C(=O)Nc2cc(Cl)cc(NS(C)(=O)=O)c2)c1
InChI InChI=1S/C18H16ClN3O3S2/c1-11-4-3-5-20-17(11)12-6-16(26-10-12)18(23)21-14-7-13(19)8-15(9-14)22-27(2,24)25/h3-10,22H,1-2H3,(H,21,23)
Molecular weight 421.03 Da
AlogP 4.395720000000003
HBond acceptors 6
HBond donors 2
Atoms 43

Expert Reviews


(on 15 Jan 2025 )
Cellular Use Rating
ATX968 is a potent inhibitor of DHX9 with expected downstream pharmacology and confirmed on-target binding by SPR. In the absence of selectivity data against other helicases or ATPases, the differentiated...
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